Article: Tegaserod

Image:Tegaserod.png
Tegaserod
Systematic (IUPAC) name
1-{[5-(hydroxymethyl)-1H-indol-3-yl]methylideneamino}- 2-pentyl-guanidine
Identifiers
CAS number	189188-57-6
ATC code	A03AE02
PubChem	5487301
DrugBank	APRD00096
Chemical data
Formula	C16H23N5O
Mol. weight	301.387 g/mol
Pharmacokinetic data
Bioavailability	10%
Protein binding	98%
Metabolism	Gastric and hepatic
Half life	11 ± 5 hours
Excretion	Fecal and renal
Therapeutic considerations
Pregnancy cat.	B3(AU) B(US)
Legal status	℞-only(US)
Routes	Oral

Tegaserod is a 5-HT₄ agonist used for the management of constipation-predominant irritable bowel syndrome (IBS). It is currently marketed by Novartis under the trade names Zelnorm® (in the US) or Zelmac (in other countries).

Tegaserod is a motility stimulant. Therapeutic effect is achieved through activation of 5-HT₄ receptors of the enteric nervous system in the gastrointestinal tract. Tegaserod stimulates gastrointestinal motility and the peristaltic reflex, and possibly also reduces abdominal pain (Rossi, 2004).